Rat intestinal sucrase inhibited by minor constituents from the leaves and twigs of Archidendron clypearia (Jack.) Nielsen

• Published in: Bioorganic & medicinal chemistry letters 2016-09, Vol.26 (17), p.4272-4276
• Main Authors: Thao, Nguyen Phuong, Luyen, Bui Thi Thuy, Vinh, Le Ba, Lee, Jung Yun, Kwon, Young In, Kim, Young Ho
• Format: Article
• Language: English
• Subjects: Animals; Archidendron clypearia; Arclysides A–B; Circular Dichroism; Fabaceae; Fabaceae - chemistry; Intestines - drug effects; Magnetic Resonance Spectroscopy; Molecular Structure; Plant Extracts - chemistry; Plant Extracts - pharmacology; Plant Leaves - chemistry; Plant Stems - chemistry; Rats; Sucrase - antagonists & inhibitors; Sucrase inhibitory activity
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2016.07.044

[Display omitted] In the search for plants, containing compounds with α-glucosidase inhibitory activity, we found that a methanolic extract from the leaves and twigs of Archidendron clypearia (Jack.) Nielsen significantly inhibited rat intestinal sucrase in vitro. A phytochemical investigation of the aqueous layer of an A. clypearia extract led to the isolation of 14 compounds (1–14). Their structures were established through extensive 1D and 2D NMR, CD data, and MS analysis. The methanolic extract, as well as the water layer at a concentration of 3.0mg/mL, showed potent sucrase inhibitory activity, with 67.78±2.53% and 95.33±2.15% inhibition, respectively. In addition, compounds 6, 7, and 10 (1.0mM) showed potent sucrase inhibition (88.36±1.15%, 81.57±1.07%, and 66.32±4.73% inhibition, respectively), which was comparable to that of the positive control, acarbose, which exhibited 89.54±0.91% inhibition. Other compounds showed moderate or weak inhibitory activity at the same concentration. The sucrase inhibitory activity of the extracts and purified compounds may provide a novel opportunity to develop a new class of antidiabetic agents.